2486-55-7Relevant academic research and scientific papers
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Paragraph 00902; 00905; 00906, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
SSTR5 ANTAGONISTS
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Paragraph 00358, (2021/06/11)
This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.
Synthesis and evaluation of novel serotonin 4 receptor radiotracers for single photon emission computed tomography
Lalut, Julien,Tournier, Benjamin B.,Cailly, Thomas,Lecoutey, Cédric,Corvaisier, Sophie,Davis, Audrey,Ballandonne, Céline,Since, Marc,Millet, Philippe,Fabis, Frédéric,Dallemagne, Patrick,Rochais, Christophe
, p. 90 - 101 (2016/04/19)
Despite its implication in several physiological and pathological processes the serotonin subtype-4 receptor (5-HT4R) has seen limited effort for the development of radiolabeling agent especially concerning single photon emission computed tomography (SPECT). Bearing an ester function, the available ligands are rapidly susceptible to hydrolysis which limits their use in vivo. In this study the synthesis of iodinated benzamide and ketone analogs were described. Their affinity for the 5-HT4R and their lipophilicity were evaluated and the most promising derivatives were evaluated ex vivo for their binding to the receptor and for their ability to displace the reference ligand [125I]-SB207710.
New compounds
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Page/Page column 17, (2009/07/10)
The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
